Nutraceuticon
Herbal Medicine is Natural Medicine
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Here we will describe our internal development of potential drug candidates for the Epidermal Growth Factor Receptor, EGFR, biomarker protein target pathway.
 
Our screening model is based on EGFR phosphorylation assay.

EGRF is a receptor tyrosine kinase which specifically phosphorylates tyrosine amino acid in proteins or peptides.  EGFR is particularily interested to cancer research related to tumors of lung, kiney, colon, neck, pancreas, bladder and breast.  EGFR is overly expressed in most tumors.  Inhibition of the activity of EGFR has direct therapeutical effect of cancer.  It is also strongly suggested that controlling the activity of EGFR can improve the efficiency of cancer drug therapy. 
 

 

 
 
 
 
Example  :
 
Source of Herbal Extracted Fractions:
 
Diabetes Formulation
Catalog # DBT001
 
 
Our screening process consists of precoated peptide substrate for EGFR in a 96 micro titer well plate.  Herbal formulation- extracted fractions are added to the assay system. The concentration effect of these herbal formulation extracts upon the kinetics of EGFR phosphorylation of the coated peptide substrate is analyzed. The extent of phosphorylation is measured by an enzyme conjugated chicken anti-phospho-tyrosine antibody, IgY-HRP. Any increase of the EGFR phosphorylation signal with the addition of herbal formulation extracts in comparison with the normal rate of EGFR phosphorylation without the herbal formulation extract is considered as enhancement of EDFR activity. 
 

 

 
 
 
The corresponding herbal formulation fraction used in the study is termed as EGFR Enhancer.  On the other hand, the decrease of phosphorylation due to the presence of the herbal formulation extracted fractions are considered as having inhibition effect on EGFR.  The herbal formulation fraction used is termed as EGFR Inhibitor.
All EGFR Inhibitors are potential cancer drug candidates which can act on the pathway related to EGFR target.  EGFR Enhancers can also help to study the functional activity of EGFR for future drug development. 
 

Over 200 fractions was extracted based on our propietary method from Diabetes Formulation #DBT001.  The first 40 fractions with various concentrations were introduced into the EGFR phosphorylation assay system.  The effect on the change of EGFR phosphorylation kinetics were plotted against the fraction number.  Three different concentrations of each fraction were used in the assay.  Value of normal EGFR activity is taken as zero baseline ( no change ).     Value of EGFR activity above zero baseline is rate enhancement.  The corresponding herbal formulation fraction is an EGFR Enhancer.  Herbal formulation fractions with decrease EGFR activity below zero are EGFR Inhibitors.    Results are shown as above. 
From above results, a number of EGFR Inhibitors are clearly available for further testing.  The EGFR Enhancers which have EGFR activity above zero have potential research interest for the understanding of the functional activity of EGFR.  These enhancers will help to drug design in the future.
 
 
 
 
 
Further Examples :
 
 
In the following study, a Lung Cancer Formulation was extracted and the initial fractions were used to study the concentration effect on EGFR activity.  Both inhibitors and enhancers were discovered.  Furthermore, Hepatitis Formulation and Tuberculosis Formulation were also extracted into water soluble fractions.  Concentration effects on EGFR using the first few fractions were also reported in the following graphs.  Similarily, both inhibitors and enhancers were discovered.  In concusion, our herbal genomics approach has discovered a large number of potential drug candidates.
   
   
   
   
   
   
 
 
Nutraceuticon, Inc.
1372 Hancock Street, Suite 303
Quincy, MA  02169
USA
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